68630-75-1

• 常用中文名：醋酸布舍瑞林
• 常用英文名：Buserelin (Acetate)
• CAS号：68630-75-1
• 分子式：C₆₂H₉₀N₁₆O₁₅
• 分子量：1239.424
• 相关类别： 原料药 激素及调节内分泌功能类药 促性激素类药
• 发布时间：2018-09-01 19:39:00
• 更新时间：2024-01-04 18:48:11
• Buserelin (INN) Acetate是一个GnRH的激动剂。

名称

• 中文名: 布舍瑞林醋酸盐
• 英文名: Buserelin acetate
• 中文别名: 醋酸布舍瑞林
• 英文别名: Buserecur; Fuset; SupreMon; 5-Oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-O-(2-methyl-2-propanyl)-D-seryl-L-leucyl-L-arginyl-N-ethyl-L-prolinamide; Suprecur-MP; 5-Oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-O-(tert-butyl)-D-seryl-L-leucyl-L-arginyl-N-ethyl-L-prolinamide; Suprafact; Receptal; EstoMal; HOE 766A; Suprecur; Itorelin; 5-Oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-O-tert-butyl-D-seryl-L-leucyl-L-arginyl-N-ethyl-L-prolinamide; L-Prolinamide, 5-oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-O-(1,1-dimethylethyl)-D-seryl-L-leucyl-L-arginyl-N-ethyl-; hoe766mp; hoe766; HOE 766MP; Profact; Buserelin (Acetate)

物化性质

• 密度: 1.4±0.1 g/cm3
• 熔点: 186-188°C
• 分子式: C₆₂H₉₀N₁₆O₁₅
• 分子量: 1239.424
• 精确质量: 1238.656006
• PSA: 475.57000
• LogP: 0.70
• 折射率: 1.671
• 储存条件: −20°C

生物活性

• 描述: Buserelin (INN) Acetate是一个GnRH的激动剂。
• 相关类别:
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> GNRH受体
  研究领域 >> 癌症
  多肽产品
• 参考文献:

  [1]. Sand E et al. Buserelin treatment to rats causes enteric neurodegeneration with moderate effects on CRF-immunoreactive neurons and Enterobacteriaceae in colon, and in acetylcholine-mediated permeability in ileum. BMC Res Notes. 2015 Dec 28;8:824.

  [2]. Jnsson A et al. Long term follow up of buserelin induced enteric neuropathy in rats. Mol Med Rep. 2016 Apr;13(4):3507-13.

  [3]. Sand E et al. Structural and functional consequences of buserelin-induced enteric neuropathy in rat. BMC Gastroenterol. 2014 Dec 11;14:209.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : OK6370000 CHEMICAL NAME : Luteinizing hormone-releasing factor (pig), 6-(O-(1,1-dimethylethyl)-D-serine)-9-(N-ethyl-L- prolinamide)-10-deglycinamide, monoacetate (salt) CAS REGISTRY NUMBER : 68630-75-1 LAST UPDATED : 199612 DATA ITEMS CITED : 16 MOLECULAR FORMULA : C60-H86-N16-O13.C2-H4-O2 MOLECULAR WEIGHT : 1299.68 HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : >400 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 33,831,1987 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : >500 mg/kg TOXIC EFFECTS : Skin and Appendages - hair REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 33,831,1987 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 36 mg/kg TOXIC EFFECTS : Behavioral - altered sleep time (including change in righting reflex) Behavioral - changes in motor activity (specific assay) Behavioral - ataxia REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 33,831,1987 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : >1 gm/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 33,831,1987 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : >1 gm/kg TOXIC EFFECTS : Skin and Appendages - hair REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 33,831,1987 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 56 mg/kg TOXIC EFFECTS : Behavioral - altered sleep time (including change in righting reflex) Behavioral - changes in motor activity (specific assay) Behavioral - ataxia REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 33,831,1987 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Mammal - dog DOSE/DURATION : >100 mg/kg TOXIC EFFECTS : Behavioral - food intake (animal) Gastrointestinal - nausea or vomiting Lungs, Thorax, or Respiration - respiratory depression REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 33,831,1987 ** REPRODUCTIVE DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 200 ug/kg SEX/DURATION : female 1 day(s) after conception TOXIC EFFECTS : Reproductive - Maternal Effects - parturition Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea) REFERENCE : YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 24,265,1996 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 40 ug/kg SEX/DURATION : female 1 day(s) after conception TOXIC EFFECTS : Reproductive - Specific Developmental Abnormalities - musculoskeletal system REFERENCE : YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 24,257,1996 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 378 gm/kg SEX/DURATION : male 9 week(s) pre-mating TOXIC EFFECTS : Reproductive - Paternal Effects - testes, epididymis, sperm duct REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 33,723,1987 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 35 gm/kg SEX/DURATION : male 5 week(s) pre-mating TOXIC EFFECTS : Reproductive - Paternal Effects - prostate, seminal vesicle, Cowper's gland, accessory glands REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 33,723,1987 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 10 ug/kg SEX/DURATION : female 6-15 day(s) after conception TOXIC EFFECTS : Reproductive - Maternal Effects - ovaries, fallopian tubes Reproductive - Maternal Effects - parturition Reproductive - Effects on Newborn - stillbirth REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 33,631,1987 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 7 ug/kg SEX/DURATION : female 15-21 day(s) after conception TOXIC EFFECTS : Reproductive - Maternal Effects - parturition Reproductive - Effects on Newborn - stillbirth REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 33,647,1987 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Implant DOSE : 1700 ug/kg SEX/DURATION : male 24 week(s) pre-mating TOXIC EFFECTS : Reproductive - Paternal Effects - spermatogenesis (incl. genetic material, sperm morphology, motility, and count) Reproductive - Paternal Effects - testes, epididymis, sperm duct REFERENCE : FESTAS Fertility and Sterility. (American Fertility Soc., 608 13th Ave. S, Birmingham, AL 35282) V.1- 1950- Volume(issue)/page/year: 57,671,1992 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 130 ug/kg SEX/DURATION : female 6-18 day(s) after conception TOXIC EFFECTS : Reproductive - Maternal Effects - ovaries, fallopian tubes Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth) Reproductive - Effects on Embryo or Fetus - extra-embryonic structures (e.g., placenta, umbilical cord) REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 33,665,1987 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 13 ug/kg SEX/DURATION : female 6-18 day(s) after conception TOXIC EFFECTS : Reproductive - Maternal Effects - ovaries, fallopian tubes Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth) REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 33,665,1987

安全

• 符号: GHS07, GHS08
• 信号词: Danger
• 危害声明: H302-H360
• 警示性声明: P201-P280-P301 + P312 + P330-P308 + P313
• 个人防护装备: Eyeshields;Faceshields;full-face particle respirator type N100 (US);Gloves;respirator cartridge type N100 (US);type P1 (EN143) respirator filter;type P3 (EN 143) respirator cartridges
• 危害码 (欧洲): T: Toxic;
• 风险声明 (欧洲): R60
• 安全声明 (欧洲): 53-22-36/37/39-45
• 危险品运输编码: NONH for all modes of transport
• WGK德国: 3
• RTECS号: OK6370000